2. Cell Cycle/DNA Damage Apoptosis
  3. CDK Apoptosis
  4. AG-012986

AG-012986 is a multitargeted CDK inhibitor. AG-012986 is active against CDK1/2/4/6/5/9, with Kis of 9.2 nM (CDK4/cyclin), 94 nM (CDK2/cyclin A), and 44 nM (CDK1/cyclin B), IC50s of 4 nM (CDK9/cyclin T) and 22 nM (CDK5/p35). AG-012986 has antiproliferative activities against cancer cells. AG-012986 induces cell cycle arrest, and apoptosis.

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AG-012986

AG-012986 Chemical Structure

CAS No. : 486414-35-1

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Based on 1 publication(s) in Google Scholar

AG-012986 Related Antibodies

Top Publications Citing Use of Products

View All CDK Isoform Specific Products:

View All Isoforms
CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

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Description

AG-012986 is a multitargeted CDK inhibitor. AG-012986 is active against CDK1/2/4/6/5/9, with Kis of 9.2 nM (CDK4/cyclin), 94 nM (CDK2/cyclin A), and 44 nM (CDK1/cyclin B), IC50s of 4 nM (CDK9/cyclin T) and 22 nM (CDK5/p35). AG-012986 has antiproliferative activities against cancer cells. AG-012986 induces cell cycle arrest, and apoptosis[1].

IC50 & Target[1]

Cdk1/cyclin B

44 nM (Ki)

cdk2/cyclin A

94 nM (Ki)

CDK4

9.2 nM (Ki)

CDK5/p35

22 nM (IC50)

CDK9/Cyclin T

4 nM (IC50)

Molecular Weight

459.51

Formula

C22H23F2N5O2S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CC=C(C=C1)NC2=NC(N)=C(S2)C(C3=C(C=CC=C3F)F)=O)N[C@@H](CN(C)C)C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (217.62 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1762 mL 10.8812 mL 21.7623 mL
5 mM 0.4352 mL 2.1762 mL 4.3525 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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In Vivo Dissolution Calculator
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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1762 mL 10.8812 mL 21.7623 mL 54.4058 mL
5 mM 0.4352 mL 2.1762 mL 4.3525 mL 10.8812 mL
10 mM 0.2176 mL 1.0881 mL 2.1762 mL 5.4406 mL
15 mM 0.1451 mL 0.7254 mL 1.4508 mL 3.6271 mL
20 mM 0.1088 mL 0.5441 mL 1.0881 mL 2.7203 mL
25 mM 0.0870 mL 0.4352 mL 0.8705 mL 2.1762 mL
30 mM 0.0725 mL 0.3627 mL 0.7254 mL 1.8135 mL
40 mM 0.0544 mL 0.2720 mL 0.5441 mL 1.3601 mL
50 mM 0.0435 mL 0.2176 mL 0.4352 mL 1.0881 mL
60 mM 0.0363 mL 0.1814 mL 0.3627 mL 0.9068 mL
80 mM 0.0272 mL 0.1360 mL 0.2720 mL 0.6801 mL
100 mM 0.0218 mL 0.1088 mL 0.2176 mL 0.5441 mL
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AG-012986 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AG-012986486414-35-1AG012986AG 012986CDKApoptosisCyclin dependent kinaseantitumorCDK inhibitionInhibitorinhibitorinhibit

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